This research will develop enzymatic methods and combined chemical and enzymatic methods for the synthesis of bioactive molecul3es. It will focus on the following programs: 1) Develop enzymatic asymmetric aldol reactions, especially for the synthesis of novel iminocyclitols for design of new enzyme inhibitors; 2) Develop new methods for synthesis of glycopeptides, glycoproteins, and sulfated glycopeptides. 3) Develop new chemicoenzymatic synthesis of the anti-cancer agents epothiolones and analogs. 4) Apply enzyme-catalyzed synthesis to tackle the problems in biochemistry and drug discovery: develop new assays, prepare glycosyltransferases enzyme substrates and inhibitors and design cell-surface sugar receptors. Significant contributions in the areas of biomedicine and synthetic organic chemistry are expected. This research program should facilitate the discovery and development of new therapeutic agents.